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Lipophilic derivatives

Kaneko, T., Kaji, K. and Matsuo, M. (1993). Protective effect of lipophilic derivatives of ascorbic acid on lipid peroxide-induced endothelial injury. Arch. Biochem. Biophys. 304, 176-180. [Pg.275]

If the photoequilibrium concentrations of the cis and trans isomers of the photoswitchable ionophore in the membrane bulk and their complexation stability constants for primary cations are known, the photoinduced change in the concentration of the complex cation in the membrane bulk can be estimated. If the same amount of change is assumed to occur for the concentration of the complex cation at the very surface of the membrane, the photoinduced change in the phase boundary potential may be correlated quantitatively to the amount of the primary cation permeated to or released from the membrane side of the interface under otherwise identical conditions. In such a manner, this type of photoswitchable ionophore may serve as a molecular probe to quantitatively correlate between the photoinduced changes in the phase boundary potential and the number of the primary cations permselectively extracted into the membrane side of the interface. Highly lipophilic derivatives of azobis(benzo-15-crown-5), 1 and 2, as well as reference compound 3 were used for this purpose (see Fig. 9 for the structures) [43]. Compared to azobenzene-modified crown ethers reported earlier [39 2], more distinct structural difference between the cis... [Pg.454]

A similar pathway involving a microwave-driven molybdenum-catalyzed asymmetric allylic alkylation as the key step was elaborated by Moberg and coworkers for the preparation of the muscle relaxant (R)-baclofen (Scheme 6.52) [108]. The racemic form of baclofen is used as a muscle relaxant (antispasmodic) lipophilic derivative of y-aminobutyric acid (GABA). Pharmacological studies have shown that the (R)-enantiomer is the therapeutically useful agonist of the GABAb receptor. Asymmetric alkylation of the allylic carbonate precursor with dimethyl malonate afforded... [Pg.142]

Another approach to this problem is a search for the other more effective spin traps. Frejaville et al. [23] demonstrated that the half-life of spin-adduct of superoxide with 5-(diethoxyphosphoryl)-5-mcthyl-l -pyrrolinc-/V-oxide (DEMPO) is about tenfold longer than that of DMPO OOH. Despite a much more efficiency of this spin trap, its hydrophilic properties limit its use for superoxide detection in lipid membranes. Stolze et al. [24] studied the efficiency of some lipophilic derivatives of DEMPO in the reaction with superoxide. These authors demonstrated a higher stability of superoxide spin-adducts with 5-(di- -propoxypho-sphoryl)-5-methyl-1 -pyrrolinc-A -oxidc (DPPMPO) and 5-(di- -butoxyphosphoryl)-5-methyl-... [Pg.964]

A variety of lipid adjuvants and protein mediators have also been shown to influence the immune response to antigens encapsulated in liposomes. The most widely used examples of such adjuvants for practical immunization procedures are endotoxin (including lipid A and lipopolysaccharide) and numerous types of lipophilic derivatives of muramyl dipeptide. [Pg.6]

Key, M.E. et al., Isolation of tumoricidal macrophages from lung melanoma metastases of mice treated systemically with liposomes containing a lipophilic derivative of muramyl dipeptide, J. Natl. Cancer Inst., 69, 1198, 1982. [Pg.166]

Sibert JW, Cory AH, Cory JC (2002) Lipophilic derivatives of cyclam as new inhibitors of tumor cell growth. Chem Commun 2 154—155... [Pg.282]

J. Nakamura, T. Miwa, Y. Mori, H. Saski, Comparative Studies on the Anticonvulsant Activity of Lipophilic Derivatives of y-Aminobutyric Acid and 2-Pyrrolidinone in Mice , J. Pharmacobio-Dynam. 1991, 14, 1-8. [Pg.250]

Turning our attention first to alkyl carbamates of cyclic amides, we find interesting attempts to improve the pharmaceutical and pharmacokinetic properties of 5-fluorouracil (8.152, R = H) [194-196], This antitumor agent, while clinically useful, suffers from poor water solubility, unsatisfactory delivery properties and low tissue selectivity. A variety of prodrug candidates were prepared, in particular the alkyl and aryl carbamates presented in Table 8.12. With the exception of the more-lipophilic derivatives, these compounds exhibited somewhat improved water solubility. More importantly, both rectal and oral bioavailability were markedly improved. The activation... [Pg.513]

Many hydroxyp5rranones and hydroxypyridinones and their metal complexes have been of importance in analytical chemistry, solvent extraction, and metal separation. Here their excellent chelating properties in conjunction with the possibility of synthesizing strongly lipophilic derivatives make this class of ligands particularly useful. [Pg.214]

Ethynylcytidine [l-(3-C-ethynyl-p-D-ribopentafuranosyl)-cytosine] (ETC) is a novel nucleoside that was foimd to be highly cytotoxic (53-55). By combination of ETC with NOAC, we synthesized the new lipophilic derivative NOAC-ETC [3 -C-ethynylcytidylyl-(5 —>5 )-N" -octadecyl-l-p-D-arabinofura-nosylcytosine]. The chemical structure of ETC-NOAC is shown in Fig. 1. [Pg.54]

Supersaxo A, et al. The antitumor effect of lipophilic derivatives of 5 -fluoro-2 -deoxyuridine incorporated into liposomes. J Microencaps 1988 5 1. [Pg.60]

Horber DH, Schott CH, Schwendener RA. Cellular pharmacology of a liposomal preparation of ISf-hexadecyl-l-P-D-arabinofuranosylcytosine, a lipophilic derivative of 1-P-D-arabinofuranosylcytosine. Br J Cancer 1995 71 957. [Pg.60]

Schwendener RA, et al. In vitro activity of liposomal N" -octadecyl-l-P-D-arabinofuranosylcytosine (NOAC), a new lipophilic derivative of 1-P-d-arabinofuranocylcytosine on biopsized clonogenic human tumour cells and haematopoietic precursor cells. Invest New Drugs 2001 19 203. [Pg.61]

T. M. Wrodnigg, S. G. Withers, and A. E. Stiitz, Novel, lipophilic derivatives of 2,5-dideoxy-2,5-imino-D-mannitol (DMDP) are powerful p-glucosidase inhibitors, Bioorg. Med. Chem. Lett., 11 (2001) 1063-1064. [Pg.284]

It is at present still difficult to correlate the absolute intensity of the SHG with the number of cationic complexes at the membrane surface. Therefore, a quantitative discussion, showing how the permselective uptake of primary cations forming SHG active complexes into the membrane side of the phase boundary corresponds to the increase in the membrane potential, is not possible yet. Lipophilic derivatives of photoswitchable azobis(benzo-15-crown-5) were recently shown as a molecular probe to determine photoinduced changes in the amount of the primary cation uptake into the membrane phase boundary in relation to the photoinduced EMF changes under otherwise identical conditions. [Pg.255]

For this puq)ose, the photoswitchable bis(crown ether)s 88 and 89 as well as the reference compound 90 have been synthesized. Compounds 88 and 89 are highly lipophilic derivatives of azobis(benzo-15-crown-5). The parent azobis crown ether was originally developed by Shinkai and its photoresponsive changes in complexation, extraction, and transport properties thoroughly examined. Compared to 87, more distinct structural difference between the cis and trans isomers can be expected for 88 and 89 because in the latter compounds the 15-crown-5 rings are directly attached to the azobenzene group. The photoequilibrium concentrations of the cis and trans forms and the photoinduced changes in the complexation constants for alkali metal ions are summarized in Table 7. [Pg.256]

Lundberg, B. (1994) The solubilization of lipophilic derivatives of podophyllotoxins in sub-micron sized lipid emulsions and their cytotoxic activity against cancer cells in cultnteJ. Pharm., 109 73-81. [Pg.224]

Uchiyama, T., Kotani, A., Tasumi, H., et al. Development of novel lipophilic derivatives of DADLE (leucine enkephalin analogue) Intestinal permeability characteristics of DADLE derivatives in rats. Pharm. Res. 17 1461-1467, 2000. [Pg.334]

Other lipophilic derivatives of EDTA and DTPA were synthesized by condensing the bisanhydride of the former with phosphatidylethanolamine to give PE-EDTA (16)121 whereas that of the latter was condensed with 11-aminoundecanoic acid to give Puchel, 17,122. PE-EDTA failed to mobilize plutonium from the hamster, although studies with PE-[14C]EDTA established the uptake of the radiolabel into the liver. [Pg.105]

Maeda H., J. Takeshita, and R. Kanamam. 1979. A lipophilic derivative of neo-carzinostatin. A polymer conjugation of... [Pg.292]

The implication for the therapeutic application of these rifampicins is quite obvious. Highly lipophilic derivatives may fail in therapy despite low in vitro MIC values (high intrinsic activity) because the time needed for the diffusion into the bacterial cell might be too long compared with their biological half-life (concentration-time profile in the serum). [Pg.191]

Some metabolic conjugative processes result in the production of lipophilic derivatives that are not readily eliminated. While their physical properties are different from the classical hydrophilic conjugates, the mechanism of formation clearly defines them as conjugates (i.e., they are formed as the result of a union of xenobiotic metabolites with endogenous molecules). The reactions involve the coupling of xenobiotic acids and alcohols with endogenous intermediates of lipid synthesis (i. e., the acids with glycerol and cholesterol and the alcohols with the fatty acids). [Pg.235]

The use of various low-water reaction systems, including anhydrous organic solvents as well as imidazolium-based ionic liquids, is investigated for the biocatalytic preparation of lipophilic derivatives of various natural phenohc compounds (Figure 9.1) including phenohc and flavonoid glycosides (escuhn, salicin, helicin. [Pg.124]


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See also in sourсe #XX -- [ Pg.18 , Pg.840 , Pg.841 , Pg.842 , Pg.843 , Pg.844 , Pg.845 , Pg.846 , Pg.847 , Pg.848 , Pg.849 , Pg.850 ]

See also in sourсe #XX -- [ Pg.840 , Pg.841 , Pg.842 , Pg.843 , Pg.844 , Pg.845 , Pg.846 , Pg.847 , Pg.848 , Pg.849 , Pg.850 ]

See also in sourсe #XX -- [ Pg.18 , Pg.840 , Pg.841 , Pg.842 , Pg.843 , Pg.844 , Pg.845 , Pg.846 , Pg.847 , Pg.848 , Pg.849 , Pg.850 ]

See also in sourсe #XX -- [ Pg.281 ]




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